Photochlor, also known as HTTP, is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.

Tildipirosin is a 16-membered macrolide used as an antibiotic in veterinary medicine. Like other macrolides, it inhibits protein synthesis in bacteria and blocks the production of biofilms.

Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

Anidulafungin

PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).

Brequinar sodium (DuP-785, Brequinar, NSC 368390) is a potent and selective inhibitor of DHODH with IC50 of 20 nM, triggers differentiation in the ER-HoxA9, U937, and THP1 cells with an ED50 of 1 uM.

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

APD597(JNJ-38431055) is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.

Sobetirome(GC-1; QRX-431) is a member of a class of compounds known as selective thyromimetics.

Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

PS48 is a PDK1 (phosphoinositide-dependent protein kinase 1) activator which binds to the HM/PIF binding pocket rather than the ATP-binding site.

FDL-169 is a novel and potent CFTR (Cystic fibrosis transmembrane conductance regulator) corrector being developed by Flatley Discovery Lab for treating cystic fibrosis (CF) patients who carry the F508del mutation

UNC2541 is a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket. UNC2541 showed IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM.

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels. It blocks the induced expression of inflammatory markers in microglial cells.

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).

FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.

FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.

CAY10594 is a potent phospholipase D2 inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.

ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.

Pindolol is a moderately lipophilic beta blocker. Pindolol is a SR-1A/SR-1B antagonist with similar affinity for each subtype. Pindolol acts as a partial agonist at mouse and human β3-AR (β3-adrenoceptors). Pindolol is an inhibitor of β1-AR.

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.

NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide (41GCWMLY46 within the N-terminus of γD-crystallin) as well as full-length γD-crystallin.

GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.

Dynasore is a cell-permeable small molecule that inhibits the GTPase activity of dynamin1, dynamin2 and Drp1, the mitochondrial dynamin.

MS-0124 is a potent and selective inhibitor of G9a-like Protein (GLP) lysine methyltransferase with IC50 of 13 nM, shows >30-fold selectivity for GLP over G9a and other methyltransferases..

Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis.

Sulfanitran is a sulfonamide antibiotic which is used in the poultry industry. It is a component of Novastat, Polystat, and Unistat, brand names of feed additives for chickens used to control Coccidioides spp.

MPC1304 is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects. IC50 & Target: Ca2+ Channel.